The equimolar complexes of vancomycin, a broad-spectrum glycopeptides antibiotic with β- cyclodextrin were prepared to evaluate their suitability for the development of a prolongedrelease form of the antibiotic. Complex preparations were subjected to kneading and freezedrying techniques and characterized using X-ray powder diffractometry (XRD), Thermogravimetric analysis (TGA), Scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FT-IR). The uniformity obtained from all of the analyzed results, suggests the successive formation of the aforementioned binary systems. The in vitro dissolution profiles of vancomycin were determined accordingly in a simulated cerebrospinal fluid where the results showed a modified release with improved bioavailabity of vancomycin was achieved upon complexation with beta-cyclodextrin. Our results therefore demonstrated that the use of cyclodextrin could be advantageous not only for lipophilic drugs but also for hydrophilic drugs.